- Design, synthesis and activity evaluation of N-(pyridin-4-yl) salicylamides as antimycobacterial agents
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A series of N-(pyridin-4-yl) salicylamides derivatives were prepared through acylation of the corresponding acetylsalicyloyl chlorides with substituted 4-amino-pyridines. These compounds were evaluated in vitro for antimycobacterial activities against Myc
- Dian, He,Zhou, De-Bin,Mou, Jian-Ping,Yang, Zhu-Qing,Zhong, Jia,Ding, Xiao-Quan,Li, Chong,Wang, Xiao-Hong,Zhang, Jian-Gang
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p. 7269 - 7275
(2015/04/22)
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- Synthesis of flavones and γ-benzopyranones using mild sonogashira coupling and 18-crown-6 ether mediated 6-endo cyclization
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An efficient method for the synthesis of flavones and γ- benzopyranones has been developed utilizing a mild Sonogashira coupling and 18-crown-6 ether mediated 6-endo cyclization of o-alkynoylphenyl acetates. By using this strategy, flavones and γ-benzopyranones bearing electron-donating groups, halogens, and simple alkyl substituents were synthesized in satisfactory yields. A facile, mild, and selective method for the synthesis of flavones and γ-benzopyranones is reported. o-Alkynoylphenyl acetates were obtained from either acyl chloride derivatives or substituted salicylates. Upon removing the acetate group, flavones and γ- benzopyranones were synthesized within 15 min with the aid of 18-crown-6 ether. A library of flavones and γ-benzopyranones was established. Copyright
- Chuang, Da-Wei,El-Shazly, Mohamed,Balaji D., Barve,Chung, Yu-Ming,Chang, Fang-Rong,Wu, Yang-Chang
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p. 4533 - 4540,8
(2020/08/31)
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- Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats
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The modification of 3′-((2-cyclopentyl-6,7-dimethyl-1-oxo-2,3- dihydro-1H-inden-5-yloxy)methyl)biphenyl-4-carboxylic acid (BINA, 1) by incorporating heteroatoms into the structure and replacing the cyclopentyl moiety led to the development of new mGluR2 positive allosteric modulators (PAMs) with optimized potency and superior druglike properties. These analogues are more potent than 1 in vitro and are highly selective for mGluR2 vs other mGluR subtypes. They have significantly improved pharmacokinetic (PK) properties, with excellent oral bioavailability and brain penetration. The benzisothiazol-3-one derivative 14 decreased cocaine self-administration in rats, providing proof-of-concept for the use of mGluR2 PAMs for the treatment of cocaine dependence.
- Dhanya, Raveendra-Panickar,Sidique, Shyama,Sheffler, Douglas J.,Nickols, Hilary Highfield,Herath, Ananda,Yang, Li,Dahl, Russell,Ardecky, Robert,Semenova, Svetlana,Markou, Athina,Conn, P. Jeffrey,Cosford, Nicholas D. P.
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experimental part
p. 342 - 353
(2011/03/18)
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- Compounds and compositions for delivering active agents
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Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.
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Page/Page column 8
(2010/11/30)
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- Structure-activity relationships of non-peptide vasopressin V(1a) antagonists: 1-(1-multi-substituted benzoyl 4-piperidyl)-3,4-dihydro-2(1H)- quinolinones
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During our systematic studies on the arginine vasopressin receptor V(1a)- antagonistic activity of 1-(1-benzoyl substituted 4-piperidyl)-3,4-dihydro- 2(1H)-quinolinones, we found a general substituent effect on the benzene ring. Hydrogen-bonding ability a
- Kondo,Ogawa,Nakaya,Tominaga,Yabuuchi
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p. 725 - 733
(2007/10/03)
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